AU6802590A - Inhibitors of retroviral proteases - Google Patents

Inhibitors of retroviral proteases

Info

Publication number
AU6802590A
AU6802590A AU68025/90A AU6802590A AU6802590A AU 6802590 A AU6802590 A AU 6802590A AU 68025/90 A AU68025/90 A AU 68025/90A AU 6802590 A AU6802590 A AU 6802590A AU 6802590 A AU6802590 A AU 6802590A
Authority
AU
Australia
Prior art keywords
glycosyl
acid
same
inhibitors
retroviral proteases
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
AU68025/90A
Other versions
AU641197B2 (en
Inventor
Karl-Heinz Budt
Anuschirwan Peyman
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sanofi Aventis Deutschland GmbH
Original Assignee
Aventis Pharma Deutschland GmbH
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Aventis Pharma Deutschland GmbH filed Critical Aventis Pharma Deutschland GmbH
Publication of AU6802590A publication Critical patent/AU6802590A/en
Application granted granted Critical
Publication of AU641197B2 publication Critical patent/AU641197B2/en
Assigned to AVENTIS PHARMA DEUTSCHLAND GMBH reassignment AVENTIS PHARMA DEUTSCHLAND GMBH Alteration of Name(s) in Register under S187 Assignors: HOECHST AKTIENGESELLSCHAFT
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
    • C07F9/5728—Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids R2P(=O)(OH); Thiophosphinic acids, i.e. R2P(=X)(XH) (X = S, Se)
    • C07F9/301—Acyclic saturated acids which can have further substituents on alkyl
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

Cpds. of formula (I) and their salts are new. - A-N(R4)-C(R2)(R3)-Q-C(R2)(R3)-N(R4)-A (I) - where Q = -P(R6)(Y-R5)-, P(R6)(NR7R7) or -S(O)m. Y = O or S. m = 1-2. A, A = -(G)p-(F)o-(E)n-D. E, F, G = a natural or synthetic amino acid, azaamino acid or imino acid. n, o, p = 0 or 1. D = R1, -CO-C(R9)(R10)-NR8-R1, CO-CH(R9)-CH(R11)-R1 or -CO-CH(R9)-O-R1. R1 = H, CO2H, opt. substd. 1-18C alkyl, or -W-R1a, where R1a is the same as R1 and W = CO, CS, OCO, SO2, SO, S, NHSO2, NHCO, CH(OH), N(OH) or CO-V, where V is a peptide residue that is 1-10 amino acids long. R1, together with R11, can form a 5-12 membered mono- or bicyclic satd. or partially unsatd. ring system that may contain an S, SO or SO2 gp. R1 may also be glycosyl (pref. glucofuranosyl or glucopyranosyl), derived from ldotetroses, aldopentoses, aldohexoses, ketopentoses, ketohexoses, deoxyaldoses, aminoaldoses, oligosaccharides and their stereoisomers. R2, R2 = the same as R1 (but is not a glycosyl gp.). R3, R3 - ( P05331)
AU68025/90A 1989-12-16 1990-12-14 Inhibitors of retroviral proteases Ceased AU641197B2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE3941607 1989-12-16
DE3941607 1989-12-16
DE4018942 1990-06-13
DE4018942 1990-06-13

Publications (2)

Publication Number Publication Date
AU6802590A true AU6802590A (en) 1991-06-20
AU641197B2 AU641197B2 (en) 1993-09-16

Family

ID=25888063

Family Applications (1)

Application Number Title Priority Date Filing Date
AU68025/90A Ceased AU641197B2 (en) 1989-12-16 1990-12-14 Inhibitors of retroviral proteases

Country Status (19)

Country Link
US (1) US5629431A (en)
EP (1) EP0435059B1 (en)
JP (1) JP2816253B2 (en)
KR (1) KR100203231B1 (en)
AT (1) ATE159946T1 (en)
AU (1) AU641197B2 (en)
CA (1) CA2032303C (en)
DE (2) DE4039569A1 (en)
DK (1) DK0435059T3 (en)
ES (1) ES2110404T3 (en)
FI (1) FI906140A (en)
GR (1) GR3025765T3 (en)
HU (1) HUT59147A (en)
IE (1) IE904516A1 (en)
IL (1) IL96677A0 (en)
NO (1) NO306552B1 (en)
NZ (1) NZ236461A (en)
PL (1) PL288270A1 (en)
PT (1) PT96180B (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5559256A (en) * 1992-07-20 1996-09-24 E. R. Squibb & Sons, Inc. Aminediol protease inhibitors

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992000954A1 (en) * 1990-07-06 1992-01-23 Smithkline Beecham Corporation Aspartic protease inhibitors
CA2127295A1 (en) * 1992-01-09 1993-07-22 Kim D. Janda Peptide linkage unit comprising methylene phosphinic acid
DE4220566A1 (en) * 1992-06-24 1994-01-20 Hoechst Ag Retroviral Protease Inhibitors
DE4310815A1 (en) * 1993-04-02 1994-10-06 Hoechst Ag New bis (aminomethyl) phosphinic acid derivatives and process for the preparation of bis (aminomethyl) phosphinic acid derivatives
AU2003242405A1 (en) 2003-05-22 2004-12-13 Lead Chemical Co., Ltd. Compounds and preparaitons having antiviral effect

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3359266A (en) * 1966-06-10 1967-12-19 Monsanto Co Process for preparing phosphorus-containing mannich bases
US4100275A (en) * 1975-01-27 1978-07-11 Hoffmann-La Roche Inc. Compositions having antibiotic properties
NZ218937A (en) * 1986-01-16 1990-03-27 Abbott Lab Functionalised peptidyl aminodiols and -triols as renin inhibitors and pharmaceutical compositions
DE3856166T2 (en) * 1987-09-29 1998-08-06 Banyu Pharma Co Ltd N-acylamino acid derivatives and their use
DE3824961A1 (en) * 1988-07-22 1990-01-25 Basf Ag Process for the preparation of bis(aminomethyl)phosphinic acid, and acidic or basic salts thereof
DE59009945D1 (en) * 1989-02-10 1996-01-18 Wolfgang Prof Dr Schramm AGENT FOR INHIBITING HIV PROTEASES.

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5559256A (en) * 1992-07-20 1996-09-24 E. R. Squibb & Sons, Inc. Aminediol protease inhibitors
US5760036A (en) * 1992-07-20 1998-06-02 E. R. Squibb & Sons, Inc. Aminediol protease inhibitors
US5776933A (en) * 1992-07-20 1998-07-07 E. R. Squibb & Sons, Inc. Method of inhibiting protease

Also Published As

Publication number Publication date
AU641197B2 (en) 1993-09-16
DE4039569A1 (en) 1991-06-20
FI906140A0 (en) 1990-12-13
CA2032303C (en) 2002-03-19
KR910011889A (en) 1991-08-07
FI906140A (en) 1991-06-17
NO306552B1 (en) 1999-11-22
PT96180B (en) 1998-05-29
IE904516A1 (en) 1991-06-19
JPH05331067A (en) 1993-12-14
NO905410L (en) 1991-06-17
US5629431A (en) 1997-05-13
DE59010771D1 (en) 1997-12-11
EP0435059B1 (en) 1997-11-05
NZ236461A (en) 1993-08-26
NO905410D0 (en) 1990-12-14
GR3025765T3 (en) 1998-03-31
ATE159946T1 (en) 1997-11-15
CA2032303A1 (en) 1991-06-17
PL288270A1 (en) 1992-08-24
HUT59147A (en) 1992-04-28
DK0435059T3 (en) 1998-07-27
KR100203231B1 (en) 1999-06-15
IL96677A0 (en) 1991-09-16
EP0435059A1 (en) 1991-07-03
ES2110404T3 (en) 1998-02-16
JP2816253B2 (en) 1998-10-27
HU908276D0 (en) 1991-06-28
PT96180A (en) 1991-09-30

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Legal Events

Date Code Title Description
PC Assignment registered

Owner name: AVENTIS PHARMA DEUTSCHLAND GMBH

Free format text: FORMER OWNER WAS: HOECHST AKTIENGESELLSCHAFT

MK14 Patent ceased section 143(a) (annual fees not paid) or expired